Abstract
The aim – to screen new solid dispersions of quercetin for the presence of antihyperglycemic action and to identify the most active substances that are promising for the creation of antidiabetic drugs.
 Materials and methods. The object of the study was 4 new solid dispersions of quercetin, developed at the National University of Pharmacy. Solid dispersions of quercetin were prepared by the liquid-phase method; hydroxypropyl methylcellulose (HPMC) or polyvinylpyrrolidone (PVP) in ratios of 1:1 and 1:2 were used as a carrier. The antihyperglycemic effect of the studied substances at a dose of 50 mg / kg was assessed in rats by the ability to lower blood glucose levels after carbohydrate loading in a model of impaired glucose tolerance induced by dexamethasone and in experimental type 2 diabetes mellitus induced by dexamethasone.
 Results. It was found that with impaired glucose tolerance, a solid dispersion of quercetin with HPMC (1:1) showed a pronounced antihyperglycemic effect – the glucose level 30 minutes after glucose load significantly decreased by 28 % and did not differ from the action of metformin, which was confirmed by the value of the area under glycemic crooked. When solid dispersions with PVP (1:1 and 1:2) were used, the antihyperglycemic effect was less pronounced. In a model of type 2 diabetes mellitus, a significant antihyperglycemic effect was found only in a solid dispersion of quercetin with HPMC (1:1) at the metformin level, which indicates an increase in the solubility and absorption of quercetin.
 Conclusions. A pronounced antihyperglycemic effect at the metformin level was found in a solid dispersion of quercetin with HPMC in a 1:1 ratio with impaired glucose tolerance and type 2 diabetes mellitus. It has been proven that a solid dispersion of quercetin with HPMC is a promising substance for creating a monocomponent drug or for inclusion in a new antidiabetic combined drug
Highlights
Diabetes mellitus, as defined by the World Health Organization, is a state of prolonged increase in blood sugar levels, which can be caused by a number of external and internal factors with the development of absolute or relative insulin deficiency, which leads to a violation of carbohydrate, fat and protein metabolism
On the 14th day in animals with control pathology, at the 30th minute of the glucose tolerance test, glycemia significantly exceeded the initial values by 2,2 times (p
The use of solid dispersions of quercetin showed that samples No 1, 3 and 4 reliably prevent the development of hyperglycemia caused by carbohydrate load (Table 2)
Summary
As defined by the World Health Organization, is a state of prolonged increase in blood sugar levels, which can be caused by a number of external and internal factors with the development of absolute or relative insulin deficiency, which leads to a violation of carbohydrate, fat and protein metabolism. According to the International Diabetes Federation (IDF), the number of patients with diagnosed diabetes mellitus among the adult population (20–79 years) in the world in 2045 will amount to 629 million [1]. Despite the constant improvement of directions in the treatment of type 2 diabetes, which prevails in the population of patients with diabetes, the achievement of normoglycemia and the prevention of chronic complications (such as retinopathy, angiopathy, neuropathy) remains a challenge, which indicates the need for the use of multicomponent method, which corresponds to the combination therapy using various groups of pharmacological agents [2]. Drug combinations with antihyperglycemic action do not always provide prevention of complications of type 2 diabetes mellitus, which indicates the relevance of the development of new combined drugs
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